Tolrestat (Synonyms: AY-27773)
目录号: PL04625 纯度: ≥99%
CAS No. :82964-04-3
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中文名称
Tolrestat
中文别名
托瑞司他;托雷斯萘;N-[[6-甲氧基-5-(三氟甲基)-1-萘基]硫代甲基]-N-甲基甘氨酸
英文名称
Tolrestat
英文别名
2-(6-Methoxy-N-methyl-5-(trifluoromethyl)naphthalene-1-carbothioamido)acetic acid;N-[[6-Methoxy-5-(trifluoromethyl)naphthalen-1-yl]thioxomethyl]-N-methylglycine;[(6-Methoxy-5-trifluoromethyl-naphthalene-1-carbothioyl)-methyl-amino]-acetic acid;2-[[6-methoxy-5-(trifluoromethyl)naphthalene-1-carbothioyl]-methylamino]acetic acid;AY-27773;Tolrestat;Alredase;N-(6-Methoxythio-5-(trifluoromethyl)-1-naphthoyl)sarcosine;Tolrestatum;Tolrestatum [Latin];CID 53359;N-[[6-Methoxy-5-(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methyl-glycine;N-[[5 -(Trifluoromethyl)-6-methoxy-lnaphthalenyl]thioxomethyl]-N-methylglycine;Tolrestatin
Cas No.
82964-04-3
分子式
C16H14NO3F3S
分子量
357.35
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Tolrestat 是一种有效的,可口服的 aldose reductase 抑制剂,IC50 值为 35 nM。
生物活性
Tolrestat is a potent, orally active aldose reductase inhibitor with IC 50 of 35 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 35 nM (Aldose Reductase)
体内研究(In Vivo)
Tolrestat (1.8 mg/kg per day) causes a reversal to normal RBC sorbitol levels diabetic rats. In 21-day diabetic rats, the estimated ID in the sciatic nerve and lenses is 4.8 and about 20 for tolrestat, and 1.7 and 2.2 for (±)sorbinil, respectively. Either tolrestat or sorbinil inhibits tissue AR activity but does not significantly affect plasma lipoprotein levels, or affect the body weight of the mice or their general health. Accumulation of cholesterol-rich foam cells is significantly increased in aortic roots of tolrestat-fed mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Sestanj K, et al. N-[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]- N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor. J Med Chem. 1984 Mar;27(3):255-6.
[2]. Simard-Duquesne N, et al. The effects of a new aldose reductase inhibitor (tolrestat) in galactosemic and diabetic rats. Metabolism. 1985 Oct;34(10):885-92.
溶解度数据
In Vitro: DMSO : 50 mg/mL (139.92 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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